| Assay ID | Title | Year | Journal | Article |
|---|
| AID723024 | Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723006 | Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723012 | Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722997 | AUC in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722999 | Mean residence time in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723025 | Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723003 | Binding affinity to human DAT at 10 uM by radioligand binding assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723023 | Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723020 | Clearance in human hepatocytes | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722994 | Antipsychotic activity in Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion at 3 mg/kg, ip after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723018 | Fraction unbound in rat plasma | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722992 | Antipsychotic activity in Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion at 30 mg/kg, ip after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722995 | Ratio of drug level in brain to plasma in rat at 10 mg/kg, ip up to 6 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID673184 | Plasma clearance in rat | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor. |
| AID722991 | Antipsychotic activity in Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion at 56.6 mg/kg, ip after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723026 | Antipsychotic activity in ip dosed Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723016 | Fraction unbound in human plasma | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723022 | Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response at 10 uM treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobi | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723000 | Volume of distribution at steady state in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723005 | Positive allosteric modulation of rat muscarinic M5 receptor assessed as acetylcholine response | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722990 | Antipsychotic activity in Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion at 100 mg/kg, ip after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722996 | Drug level in rat brain at 10 mg/kg, ip up to 6 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723004 | Binding affinity to rat GABAA receptor at 10 uM by radioligand binding assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723007 | Positive allosteric modulation of rat muscarinic M3 receptor assessed as acetylcholine response | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723017 | Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723002 | Clearance in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723021 | Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response at 10 uM relative to acetylcholine | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723014 | Positive allosteric modulation of rat muscarinic M1 receptor assessed as acetylcholine response | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723008 | Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722993 | Antipsychotic activity in Sprague-Dawley rat assessed as reversal of amphetamine-induced hyperlocomotion at 10 mg/kg, ip after 90 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID722998 | Systemic plasma concentration in rat at 10 mg/kg, ip up to 6 hrs | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723019 | Clearance in rat hepatocytes | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723001 | Half life in rat at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID723010 | Positive allosteric modulation of rat muscarinic M2 receptor assessed as acetylcholine response | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |